METHOD OF PRODUCING 3-(2-ALKYNYL)-1,3-OXAZOLIDINES Russian patent published in 2015 - IPC C07D263/04 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, particularly to a method of producing 3-(2-alkynyl)-1,3-oxazolidines of formula (1) where R¹=R²=H; R³=n-Pr(a), n-Bu (b), Ph (c); R¹=CH₃, R²=H, R³=n-Pr (d), n-Bu (e), Ph (f); R¹=H, R²=CH₂CH₃, R³=n-Pr (g), n-Bu (h), Ph (i); R¹=Ph, R²=H, R³=Ph (k), which can be used as universal precursors for fine organic synthesis and biologically active compounds. The method is carried out by reacting monoethanolamine of general formula HO(R¹)CHCH(R²)NH₂ (where R¹=R²=H; R¹=CH₃, R²=H; R¹=H, R²=CH₂CH₃; R¹=Ph, R²=H) with paraform while boiling in benzene for 5 hours, followed by evacuating benzene and adding alkyl(phenyl)acetylene-1 of general formula R³-C≡CH (where R³=C₃H₅, C₄H₉, Ph) in toluene and a CuCl catalyst. The reaction mass is mixed in an argon atmosphere at 80°C and atmospheric pressure for 5-7 hours. The reaction is carried out in molar ratio HO(R¹)CHCH(R²)NH₂: (CH₂O)_n: R³-C≡CH: CuCl=2:3:1:(0.03-0.07).

EFFECT: selective production of said compounds.

1 tbl, 14 ex